Evangelisti Giulio, Barra Fabio, Perrone Umberto, Di Donato Nadine, Bogliolo Stefano, Ceccaroni Marcello, Ferrero Simone
Academic Unit of Obstetrics and Gynecology, IRCCS Ospedale Policlinico San Martino, Genoa, Italy.
Southern Endometriosis Centre, Queen Alexandra Hospital, Portsmouth, UK.
Expert Opin Drug Metab Toxicol. 2022 Jul-Aug;18(7-8):441-457. doi: 10.1080/17425255.2022.2113381. Epub 2022 Aug 23.
Uterine fibroids are the most common benign gynecological tumors affecting women of reproductive ages. Although surgery is the definitive treatment choice, several medical approaches have been investigated to control their symptoms. The main issue of currently employed drugs for uterine fibroids is the long-term safety and tolerability profile. Today, new emerging options represent hopeful alternatives that could potentially overcome these limitations.
This manuscript aims to give an updated overview of the pharmacodynamic and pharmacokinetic properties of current and new investigational medical drugs for the treatment of symptomatic uterine fibroids. The bibliographic research was conducted by searching alone or combined keywords on the following electronic databases: Medline, PubMed, Embase, Science Citation Index via Web of Science.
The most recent therapeutic strategies for uterine fibroids are represented by gonadotropin-releasing hormone antagonists (GnRH-ants; elagolix and relugolix) and selective progesterone receptor modulators (SPRM; ulipristal acetate). After early promising results, studies on innovative drugs, such as linzagolix (GnRH-ant) and vilaprisan (SPRM) are demanding. In the near future, a deeper knowledge of biological mechanisms at the basis of the genesis and growth of uterine fibroids could pave the way for the development of innovative targeted therapies.
子宫肌瘤是影响育龄女性的最常见妇科良性肿瘤。尽管手术是最终的治疗选择，但人们已研究了多种医学方法来控制其症状。目前用于治疗子宫肌瘤的药物的主要问题是长期安全性和耐受性。如今，新出现的选择代表了有望克服这些局限性的替代方案。
本手稿旨在对当前及新研究的用于治疗有症状子宫肌瘤的药物的药效学和药代动力学特性进行最新概述。通过在以下电子数据库中单独或组合搜索关键词进行文献研究：Medline、PubMed、Embase、通过科学网的科学引文索引。
子宫肌瘤的最新治疗策略以促性腺激素释放激素拮抗剂（GnRH拮抗剂；艾拉戈利克和瑞卢戈利克）和选择性孕激素受体调节剂（SPRM；醋酸乌利司他）为代表。在取得早期有前景的结果后，对创新药物如林扎戈利克（GnRH拮抗剂）和维拉普瑞森（SPRM）的研究备受关注。在不久的将来，对子宫肌瘤发生和生长基础的生物学机制的更深入了解可能为创新靶向治疗的发展铺平道路。
